公开(公告)号：EP1155019B1

公开(公告)日：2005-12-07

申请号：EP00905776.1

申请日：2000-01-25

申请人： National Jewish Medical and Research Center ,  Aeolus Sciences, Inc. ,  Duke University

发明人： CRAPO, James D. National Jewish Med. & Res. Ctr. ,  DAY, Brian J. National Jewish Medical & Res. Ctr. ,  TROVA, Michael P. Albany Molecular Research, Inc. ,  GAUUAN, Polivini Jolicia F. ,  KITCHEN, Douglas B. ,  FRIDOVICH, Irwin ,  BATINIC-HABERLE, Ines

IPC分类号： C07D487/02 ,  C09B47/00 ,  A61K51/02 ,  A61P29/00 ,  A61P39/06 ,  A61P11/06

CPC分类号： A61K31/555 ,  A61K31/409 ,  C07D487/22 ,  C09B47/00

摘要： The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.

公开(公告)号：EP1543007A1

公开(公告)日：2005-06-22

申请号：EP03765680.8

申请日：2003-07-18

申请人： Montana State University

发明人： DRATZ, Edward, A. ,  GRIECO, Paul, A.

IPC分类号： C07D487/02

CPC分类号： C07F5/022 ,  G01N33/533 ,  G01N33/582

摘要： The invention relates to compositions and methods useful in the labeling and identification of proteins. The invention provides for highly soluble zwitterionic dye molecules where the dyes and associated side groups are non-titratable and maintain their net zwitterionic character over a broad pH range, e.g. between pH 3 and 12. These dye molecules find utility in a variety of applications, including use in the field of proteomics.

公开(公告)号：EP1458383A4

公开(公告)日：2005-05-25

申请号：EP02794267

申请日：2002-12-13

申请人： MERCK & CO INC

发明人： COSFORD NICHOLAS D P ,  CHEN CHIXU ,  EASTMAN BRIAN W ,  HUANG DEHUA ,  MUNOZ BENITO ,  PRASIT PETPIBOON ,  SMITH NICHOLAS D ,  HU ESSA

IPC分类号： A61K31/4155 ,  A61K31/424 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K45/00 ,  A61P3/04 ,  A61P17/06 ,  A61P21/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P29/00 ,  A61P43/00 ,  C07D231/38 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  A61K31/437 ,  A61P25/00 ,  C07D401/06 ,  C07D487/02

CPC分类号： C07D231/38 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

公开(公告)号：EP1214075B1

公开(公告)日：2004-06-16

申请号：EP00957941.8

申请日：2000-09-01

申请人： Neurocrine Biosciences, Inc.

发明人： THIELE, William, J. ,  O'DONNELL, Patrick, B.

IPC分类号： A61K31/519 ,  C07D487/02 ,  C07D487/04 ,  A61K31/505

CPC分类号： C07D487/04

摘要： Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (Compound (1)), and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Processes for making the same, as well as related compositions and methods are also disclosed, particularly with regard to treatment of insomnia. A polymorph Form (I) possessing exception physical and heat stability is provided. A polymorph Form II.

公开(公告)号：EP1425029A1

公开(公告)日：2004-06-09

申请号：EP02768507.2

申请日：2002-08-12

申请人： Palatin Technologies, Inc.

发明人： SHARMA, Shubh, D. ,  SHI, Yiqun ,  RAJPUROHIT, Ramesh ,  WU, Zhijun

IPC分类号： A61K38/00 ,  G01N31/00 ,  G01N33/53 ,  G06F19/00 ,  C07K1/00 ,  C07K14/00 ,  C07D207/00 ,  C07D209/02 ,  C07D241/04 ,  C07D295/00 ,  C07D487/02

CPC分类号： C07D487/04 ,  A61K38/12 ,  C07D207/16 ,  C07D241/04 ,  C07D241/08 ,  C07D317/72 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/12 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06078 ,  C07K5/06191 ,  C07K5/081 ,  C07K5/0821 ,  C07K5/0823 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/101 ,  G06F19/16 ,  G06F19/706

摘要： The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residu, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-,6 and 8-membered and 5-5 and 6-5 bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.

公开(公告)号：EP1326846A1

公开(公告)日：2003-07-16

申请号：EP01977866.1

申请日：2001-10-01

申请人： Merck & Co., Inc.

发明人： MCWILLIAMS, James Christopher ,  BUCK, Elizabeth ,  ENG, Kan, K. ,  MALIGRES, Peter, E. ,  SAGER, Jess, W. ,  WATERS, Marjorie See ,  HUMPHREY, Guy, R.

IPC分类号： C07D239/02 ,  C07D401/00 ,  C07D471/02 ,  C07D487/02

CPC分类号： C07D471/04

摘要： A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of αvβ3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.

公开(公告)号：EP1326615A1

公开(公告)日：2003-07-16

申请号：EP01977309.2

申请日：2001-10-01

申请人： Merck & Co., Inc.

发明人： MEISSNER, Robert, S. ,  XU, Wei

IPC分类号： A61K31/55 ,  A61P19/10 ,  C07D487/02

CPC分类号： C07D471/04 ,  A61K31/55

摘要： The phosphoric acid salt of 3-(2-methoxy-pyrimidin-5-yl)-5-oxo-9-(6,7,8,9-tetrahydro-5H-pyrido[2,3-b]azepin-2-yl)-nonanoic acid is a potent antagonist of the integrin αξβ3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions and methods of use.

公开(公告)号：EP1254116A1

公开(公告)日：2002-11-06

申请号：EP01908643.8

申请日：2001-01-19

申请人： Merck & Co., Inc.

发明人： ASKEW, Ben, C. ,  BRESLIN, Michael, J. ,  DUGGAN, Mark, E. ,  HUTCHINSON, John, H. ,  MEISSNER, Robert, S. ,  PERKINS, James, J. ,  STEELE, Thomas, G. ,  PATANE, Michael, A.

IPC分类号： C07D213/02 ,  C07D233/04 ,  C07D233/14 ,  C07C233/16 ,  C07D239/02 ,  C07D265/36 ,  C07D471/02 ,  C07D487/02 ,  A61K31/40 ,  A61K31/44 ,  A61K31/55 ,  A61K31/415 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D239/26 ,  C07D239/42 ,  C07D239/48 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

摘要翻译： 本发明涉及新的链烷酸衍生物，它们的合成，以及它们作为αv整联蛋白受体拮抗剂的用途。 更具体地说，本发明化合物是整联蛋白受体αvβ3和/或αβ5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，抑制血管再狭窄，糖尿病性视网膜病，黄斑变性，血管生成，动脉粥样硬化，炎性关节炎 ，癌症和转移性肿瘤生长。

公开(公告)号：EP0958279A4

公开(公告)日：2002-10-09

申请号：EP98907517

申请日：1998-02-18

申请人： CRYOVAC INC

发明人： BANSLEBEN DONALD ALBERT ,  FRIEDRICH STEFAN K ,  YOUNKIN TODD ROSS ,  GRUBBS ROBERT HOWARD ,  WANG CHUNMING ,  LI ROBERT TAN

IPC分类号： C07D263/14 ,  B01J31/14 ,  B01J31/18 ,  B01J31/22 ,  B01J31/24 ,  C07C249/02 ,  C07C251/24 ,  C07F7/18 ,  C07F9/50 ,  C07F15/04 ,  C08F4/64 ,  C08F4/70 ,  C08F4/80 ,  C08F10/00 ,  C07D207/00 ,  B01J31/00 ,  C07D209/00 ,  C07D487/02 ,  C07D491/02 ,  C07D495/02 ,  C07D497/02 ,  C08F4/00

CPC分类号： B01J31/2404 ,  B01J31/143 ,  B01J31/1805 ,  B01J2531/824 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07C249/02 ,  C07C2603/24 ,  C07C2603/26 ,  C07F15/045 ,  C08F10/00 ,  C08F110/02 ,  C08F4/64048 ,  C08F4/659 ,  C08F4/26 ,  C08F4/80 ,  C08F2500/10 ,  C08F2500/03 ,  C08F4/7022

摘要： The present invention is directed to certain novel late transition metal salicylaldimine chelates and, further, to novel bidentate ligand compounds of substituted salicylaldimine, and their utility as polymerization catalysts alone or in combination with adjunct agent and/or Lewis base in processes of polymerizing olefin monomers and copolymerizing olefin monomers with functionalized olefin monomers.

摘要翻译： 本发明涉及烯烃聚合方法和烯烃与官能化烯烃在下式表示的某些后期过渡金属二齿水杨醛亚胺螯合物存在下的共聚合：其中每个符号R，R 1，R 2，R 3，R 4，R 5 R6，L，M，A，X和Z在下面的说明书中定义。

公开(公告)号：EP0917529A4

公开(公告)日：2002-10-02

申请号：EP98908596

申请日：1998-02-18

申请人： CRYOVAC INC

发明人： BANSLEBEN DONALD ALBERT ,  FRIEDRICH STEFAN K ,  YOUNKIN TODD ROSS ,  GRUBBS ROBERT HOWARD ,  WANG CHUNMING ,  LI ROBERT TAN

IPC分类号： B01J31/14 ,  B01J31/18 ,  B01J31/24 ,  C07C2/36 ,  C07D207/32 ,  C07D207/335 ,  C07D209/14 ,  C07D209/52 ,  C07F7/00 ,  C07F7/28 ,  C07F15/00 ,  C07F15/02 ,  C07F15/04 ,  C07F15/06 ,  C08F4/42 ,  C08F4/60 ,  C08F10/00 ,  C07D207/00 ,  B01J31/00 ,  C07D209/00 ,  C07D487/02 ,  C07D491/02 ,  C07D495/02 ,  C07D497/02 ,  C08F4/00

CPC分类号： C08F10/00 ,  B01J31/143 ,  B01J31/1815 ,  B01J31/2404 ,  B01J2231/12 ,  B01J2231/122 ,  B01J2231/20 ,  B01J2531/824 ,  B01J2531/847 ,  C07C2/36 ,  C07C2531/24 ,  C07D207/335 ,  C07F15/04 ,  C08F4/659 ,  C08F4/7021 ,  C08F4/80

摘要： The present invention is directed to certain novel late transition metal pyrrolaldimine chelates and, further, to novel bidentate ligand compounds of substituted pyrrolaldimine, and their utility as polymerization catalysts in processes of polymerizing olefin monomers and copolymerizing olefin monomers with functionalized alpha-olefin monomers.